• Title/Summary/Keyword: polymeric micelle

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Drug Release from Thermo-Responsive Self-assembled Polymeric Micelles Composed of Cholic Acid and Poly(N-isopropylacrylamide)

  • Kim, In-Sook;Jeong, Young-Il;Lee, Yun-Ho;Kim, Sung-Ho
    • Archives of Pharmacal Research
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    • v.23 no.4
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    • pp.367-373
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    • 2000
  • Cholic acid, conjugated with amine-terminated poly(W-isopropylacrylamide) (abbreviated as CA/ATPNIPAAm), was synthesized by a N, N'-dicyclohexyl carbodiimide (DCC)-mediated coupling reaction. Self-assembled CA/ATPNIPAAm micelles were prepared by a diafiltration method in aqueous media. The CA/ATPNIPAAm micelles exhibited a lower critical solution temperature (LCST) at $31.5^{\circ}C$. Micelle sizes measured by photon correlation spectroscopy (PCS) were approximately 31.6 $\times$$\times$ 5.8 nm. The CA/ATPNIPAAm micelles were spherical and their thermal size transition was observed by transmission electron microscope (TEM). A fluorescence probe technique was used for determining the micelle formation behavior of CA/ATPNIPAAm in aqueous solutions using Pyrene as a hydrophobic Probe. The critical micelle concentration (CMC) was evaluated as $8.9{\times}0^{-2}$ g/L. A drug release study was performed using indomethacin (IN) as a hydrophobic model drug. The release kinetics of IN from the CA/ATPNIPAAm micelles revealed a thermo-sensitivity by the unique character of poly(N-isopropylacrylamide) i.e. the release rate was higher at $25^{\circ}C$ than at $37^{\circ}C$.

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Waterborne Core-shell Pressure Sensitive Adhesive (PSA) Based on Polymeric Nano-dispersant (고분자 분산제를 이용한 Core-shell 수성 감압점착제)

  • Lee, Jin-Kyoung;Chin, In-Joo
    • Journal of Adhesion and Interface
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    • v.17 no.3
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    • pp.89-95
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    • 2016
  • An environmentally friendly water-based pressure sensitive adhesive (PSA) was designed in an attempt to replace the solvent-based adhesive for dry lamination used in flexible food packaging films. Instead of using a low molecular weight surfactant, which may have variable material properties, a high molecular weight dispersant was used for emulsification. A polymeric nano-dispersant (PND) was synthesized using solution polymerization, and it was used as a micelle seed in the surfactant, resulting in the synthesis of a core/shell grafted acrylic adhesive. The shell and core exhibited different $T_g$ values, so that the initial adhesion strength and holding power were complemented by the film's flexibility, which is required to provide good adhesion of thin films. Results showed that the PSA designed in this study using the PND instead of traditional low molecular weight surfactant had adhesive properties applicable to the flexible packaging with appropriate tack.

Effect of Polymeric Surfactant on the Separation of 1-Naphthylamine by Micellar Enhanced Ultrafiltration Membranes (고분자형 계면활성제가 마이셀 촉진 한외여과법에 의한 1-나프틸 아민의 제거에 미치는 영향)

  • Youngkook Choi;Soobok Lee;Minok Koo;Yutaka Ishigami;Toshio Kajiuchi
    • Membrane Journal
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    • v.7 no.3
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    • pp.131-135
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    • 1997
  • Polymeric micellar enhanced ultrafiltration method using a new type of polyrmer, $\alpha$-allyl-$\omega$-methoxy polyoxyethlene and maleic anhydride copolymer (AKM-0531, Mw 15, 000), has been proposed to separate 1-naphthylamine as a weak cationic toxic organic solubilizate. Enhancement effect of polymeric micelle was identified by the ultrafiltration runs using polyacryronitrile(PAN) holow fiber membrane with molecular weight cut off 6, 000. The linear dependance of flux on the pressure difference is shown to be valid up to 0.6kg/${cm}^2$ and the rate of flux increase in response to change in the pressure is gradually reduced under the pressure difference. Rejection of 0.96 was observed for f mM of 1-naphthylamine with 2 wt.% polymer solution at the conditions of 0.4kg/${cm}^2$, natural pH. and $25^{\circ}C$ Solubilization of 1-naphthylamine into the polymeric micelle enhanced the separation efficiency.

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Poly(benzyl-L-histidine)-b-Poly(ethylene glycol) Micelle Engineered for Tumor Acidic pH-Targeting, in vitro Evaluation

  • Lee, Eun-Seong;Youn, Yu-Seok
    • Bulletin of the Korean Chemical Society
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    • v.29 no.8
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    • pp.1539-1544
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    • 2008
  • A polymeric micelle, based on the poly(benzyl-L-histidine)-b-poly(ethylene glycol) (polyBz-His-b-PEG) diblock copolymer, was designed as a tumor-specific targeting carrier. The micelles (particle size: 67-80 nm, critical micelle concentration (CMC); 2-3 $\mu$g/mL) were formed from the diafilteration method at pH 7.4, as a result of self-assembly of the polyBz-His block at the core and PEG block on the shell. Removing benzyl (Bz) group from polyBz-His block provided pH-sensitivity of the micellar core; the micelles were physically destabilized in the pH range of pH 7.4-5.5, depending on the content of the His group free from Bz group. The ionization of His group at a slightly acidic pH promoted the deformation of the interior core. These pHdependent physical changes of the micelles provide the mechanism for pH-triggering anticancer drug (e.g., doxorubicin: DOX) release from the micelle in response to the tumor’s extracellular pH range (pH 7.2-6.5).

Preparation of Polymeric Self-Assembly and Its Application to Biomaterials

  • Cho, Chong-Su;Park, In-Kyu;Nah, Jae-Woon;Toshihiro Akaike
    • Macromolecular Research
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    • v.11 no.1
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    • pp.2-8
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    • 2003
  • The self-assembly of polymers can lead to supramolecular systems and is related to the their functions of material and life sciences. In this article, self-assembly of Langmuir-Blodgett (LB) films, polymer micelles, and polymeric nanoparticles, and their biomedical applications are described. LB surfaces with a well-ordered and layered structure adhered more cells including platelet, hepatocyte, and fibroblast than the cast surfaces with microphase-separated domains. Extensive morphologic changes were observed in LB surface-adhered cells compared to the cast films. Amphiphilic block copolymers, consisting of poly(${\gamma}$-benzyl L-glutamate) (PBLG) as the hydrophobic part and poly(ethylene oxide) (PEO) [or poly(N-isopropylacrylamide) (PNIPAAm)] as the hydrophilic one, can self-assemble in water to form nanoparticles presumed to be composed of the hydrophilic shell and hydrophobic core. The release characteristics of hydrophobic drugs from these polymeric nanoparticles were dependent on the drug loading contents and chain length of the hydrophobic part of the copolymers. Achiral hydrophobic merocyanine dyes (MDs) were self-assembled in copolymeric nanoparticles, which provided a chiral microenvironment as red-shifted aggregates, and the circular dichroism (CD) of MD was induced in the self-assembled copolymeric nanoparticles.

Fabrication of Compound K-loaded Polymeric Micelle System and its Characterization in vitro and Oral Absorption Enhancement in vivo

  • Hong, Sun-Mi;Jeon, Sang-Ok;Seo, Jo-Eun;Chun, Kyeung-Hwa;Oh, Dong-Ho;Choi, Young Wook;Lee, Do Ik;Jeong, Seong Hoon;Kang, Jae Seon;Lee, Sangkil
    • Bulletin of the Korean Chemical Society
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    • v.35 no.11
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    • pp.3188-3194
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    • 2014
  • Compound K (CK) was formulated as polymeric micelles (PM) using Pluronic$^{(R)}$ F-127 to enhance the oral absorption of CK, an intestinal bacterial metabolite of ginseng protopanaxadiol saponin. The physicochemical properties of Ck-loaded PM were characterized and an in vitro transport study using the Caco-2 cell system as well as an in vivo pharmacokinetic study using SD rats was carried out. The hydrodynamic mean particle size of CK-loaded PM (CK-PM) was $254{\pm}23.45nm$ after rehydration and the drug loading efficiency was ca. 99.9%. The FT-IR spectroscopy, X-ray diffraction, differential scanning calorimetry and scanning electron microscopy data supported the presence of a new solid phase in the PM. The $P_{app}$ value of in vitro Caco-2 cell permeation of CK-PM and the oral absorption of CK was enhanced about 1.2-fold and 2.6-fold compared to CK suspension, respectively, showing that the present PM formulation enabled an enhancement of oral CK absorption.

Improved Dissolution Characteristics of Silymarin and Their Bioavailability in Rats (실리마린의 용출개선 및 흰쥐에서의 생체이용률 평가)

  • Kim, Jeong-Hoon;Jang, Sun-Woo;Kweon, Jong-Weon;Kim, Won-Bae;Choi, Yong-Wook
    • Journal of Pharmaceutical Investigation
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    • v.33 no.1
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    • pp.61-65
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    • 2003
  • Silybin is the main component of Cardus marianus extracts originated from Silybum marianum and has a hepato-protective effect. It is a water-insoluble compound and poorly absorbed from the gastrointestinal tract, resulting in very low oral bioavailability(BA). Polymeric mixed-micelle precursor formulation was made to enhance the dissolution rate of silybin, showing the results of pH-independent release profile with increased dissolution. Oral BA of different preparations in rats was evaluated, revealing that the new formulation showed increased BA more than 2-fold and 4-fold compared to the marketed product and Cardus marianus extracts itself, respectively.

Ultra pH-Sensitive Polymeric Nanosystems for Tumor Targeting and chemotherapy

  • Lee, Eun-Seong;Na, Kun;Bae, You-Han
    • Proceedings of the Polymer Society of Korea Conference
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    • 2006.10a
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    • pp.56-57
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    • 2006
  • The ultra pH-sensitive polymeric mixed micelles based on poly(L-histidine) chemistry and constructed from block copolymers containing polyHis, present four functionalities as decreasing pH: ligand exposure at pH 7.0, micelle destabilization below pH 6.8, enhanced DOX release and endosomal membrane disruption. The first functionality is expected to endow tumor pH specificity to nonspecific ligands and the rest ones may help to treat solid tumors that are hard-to-treat by conventional chemotherapy (resistant tumors). The concept was proven in vitro studies and in vivo model.

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Synthesis and Characterization of Poly(alkyl $\alpha$, L-glutamate-co-ethylene oxide)

  • Kim, Gunwoo;Kim, Jin-Yeol;Daewon Sohn;Lee, Youngil
    • Macromolecular Research
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    • v.10 no.1
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    • pp.49-52
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    • 2002
  • Rod-coil amphiphilic block copolymers, PALG-PEOs, poly(alkyl $\alpha$, L-glutamate-co-ethylene oxide)s, were successfully synthesized in three steps: 1) esterification of L-glutamic acid, 2) synthesis of ${\gamma}$-alkyl L-gultamate N-carboxyanhydride, and 3) polymerization of NCA monomers. These molecules form polymeric micelles with the hydrophobic core and hydrophilic corona in aqueous solution, which were characterized by light scattering and static fluorescence measurement.